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说明： Potent and selective cdk inhibitor; orally bioavailable
化学名： [4-Amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)methanone
纯度： ≥98% (HPLC)
生物活性 for R 547
R 547 is a potent and selective CDK inhibitor (Ki values are 1, 2, 3, 46, 171 and 260 nM for CDK4/cyclin D1, CDK1/cyclin B, CDK2/cyclin E, GSK3α, CDK7/cyclin H and GSK3β). Exhibits no effect against a panel of >120 other kinases (Ki > 5,000 nM). Inhibits the proliferation of tumor cell lines independent of multidrug resistant status, or p53 status. Suppresses retinoblastoma protein in tumor cells and xenografts. Also inhibits tumor growth in the HCT116 human colorectal tumor xenograft model in nude mice. Orally bioavailable.
技术数据 for R 547
| 分子量 | 441.45 |
| 公式 | C18H21F2N5O4S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 741713-40-6 |
| PubChem ID | 6918852 |
| InChI Key | JRNJNYBQQYBCLE-UHFFFAOYSA-N |
| Smiles | FC1=C(C(C2=C(N)N=C(NC3CCN(S(C)(=O)=O)CC3)N=C2)=O)C(OC)=CC=C1F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for R 547
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.15 | 100 |
制备储备液 for R 547
以下数据基于产品分子量 441.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.33 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.53 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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产品说明书 for R 547
参考文献 for R 547
参考文献是支持产品生物活性的出版物。
Chu et al (2006) Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. J.Med.Chem. 49 6549 PMID: 17064073
DePinto et al (2006) In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol.Cancer Ther. 5 2644 PMID: 17121911
If you know of a relevant reference for R 547, please let us know.
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关键词: R 547, R 547 supplier, R547, Cyclin-dependent, protein, kinases, inhibitors, inhibits, potent, selective, cdk, Cdk1, cdk2, cdk3, cdk4, cyclin, D1, B, E, orally, bioavailable, Kinase, Non-selective, CDKs, 5494, Tocris Bioscience
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